| Synthesis and antitumor activity of novel thermosensitive platinum(II)-cyclotriphosphazene conjugates. | |
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MedLine Citation:
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PMID: 12880697 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Thermosensitive cyclotriphosphazenes bearing alkoxy poly(ethylene glycol) and amino acid esters as side groups could be functionalized to chelate the antitumor (diamine)platinum(II) moiety through the dicarboxylate group of the amino acid substituent on the cyclic phosphazene ring. Surprisingly, like the precursor cyclotriphosphazenes, these (diamine)platinum(II)-cyclotriphosphazene conjugates were also found to exhibit variable lower critical solution temperatures (LCST) in the wide range of 12 to 92 degrees C. Furthermore, the present conjugates have shown outstanding in vitro and in vivo antitumor activities due to controlled release of the antitumor (diamine)platinum(II) moiety with hydrolytic degradation of the phosphazene ring. A few of these conjugates have shown LCSTs below body temperature, and it has been shown from a model animal experiment that the conjugates with a LCST below body temperature may be applied to local drug delivery by direct intratumoral injection. |
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Authors:
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Soo-Chang Song; Sang Beom Lee; Bae Hoon Lee; Hyung-Wook Ha; Kyung-Tae Lee; Youn Soo Sohn |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of controlled release : official journal of the Controlled Release Society Volume: 90 ISSN: 0168-3659 ISO Abbreviation: J Control Release Publication Date: 2003 Jul |
Date Detail:
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Created Date: 2003-07-25 Completed Date: 2004-01-12 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 8607908 Medline TA: J Control Release Country: Netherlands |
Other Details:
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Languages: eng Pagination: 303-11 Citation Subset: IM |
Affiliation:
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Division of Life Science, Korea Institute of Science & Technology, 130-650 Seoul, South Korea. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Antineoplastic Agents / chemical synthesis*, chemistry, pharmacology Body Temperature Cell Line, Tumor Chemistry, Pharmaceutical Drug Carriers Drug Compounding Drug Screening Assays, Antitumor Magnetic Resonance Spectroscopy Mice Organophosphorus Compounds / chemical synthesis*, chemistry, pharmacology Organoplatinum Compounds / chemical synthesis*, chemistry, pharmacology Structure-Activity Relationship Temperature |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents; 0/Drug Carriers; 0/Organophosphorus Compounds; 0/Organoplatinum Compounds |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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